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31. 发明授权

US3953417A Synthetically modified trypsin inhibitors and process for preparing them 失效
标题翻译：合成修饰的胰蛋白酶抑制剂及其制备方法
公开(公告)号：US3953417A
公开(公告)日：1976-04-27
申请号：US503066
申请日：1974-09-04
申请人： Wolfgang Konig , Oswald Zwisler , Gerhard Guthorlein
发明人： Wolfgang Konig , Oswald Zwisler , Gerhard Guthorlein
IPC分类号： C07K14/00 , A61K38/55 , C07K1/107 , C07K5/093 , C07K5/113 , C07K7/06 , C07K14/81 , C07C103/52 , C08H1/00
CPC分类号： C07K5/0819 , C07K1/1075 , C07K5/1021 , Y02P20/55 , Y10S930/29
摘要： Modified trypsin-callicrein inhibitor wherein the five carboxyl groups present in the unmodified material are amidated by--(R)(R).sub.X W groups,Wherein R is prolyl or ##EQU1## X is an integer from 1 to 10, Y is hydrogen, alkyl, or substituted alkyl and W is --OH, --NH.sub.2, --NHC.sub.2 H.sub.5, --OCH.sub.3, or --OC.sub.2 H.sub.5. Method for making trypsin-callicrein inhibitor so modified by amidation.
摘要翻译：存在于未修饰材料中的五个羧基的修饰的胰蛋白酶 - 呼丝丝素抑制剂被 - （R）（R）XW基团酰胺化，WHEREIN R是脯氨酰基或-NH-CH-CO-，| YX是1至10的整数 Y是氢，烷基或取代的烷基，W是-OH，-NH 2，-NHC 2 H 5，-OCH 3或-OC 2 H 5。通过酰胺化修饰胰蛋白酶 - 呼丝菌素抑制剂的方法。

32. 发明授权

US5466669A Immunostimulatory agent 失效
标题翻译：免疫刺激剂
公开(公告)号：US5466669A
公开(公告)日：1995-11-14
申请号：US971981
申请日：1993-02-19
申请人： Wolfgang Konig , Mamoru Tomita , Seiichi Shimamura , Kozo Kawase , Mitsunori Takase , Wayne R. Bellamy
发明人： Wolfgang Konig , Mamoru Tomita , Seiichi Shimamura , Kozo Kawase , Mitsunori Takase , Wayne R. Bellamy
IPC分类号： A61K38/16 , A61K8/64 , A61K38/00 , A61P37/04 , A61Q11/00 , A61Q19/00 , C07K14/475 , C07K14/79 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07K14/79 , A61K8/64 , A61Q19/00 , A61K38/00 , A61Q11/00
摘要： There is disclosed an immunostimulatory agent comprising a peptide derived from lactoferrin having activity to modulate the release of inflammatory mediators from cells of the immune system. The peptide promotes the release of leukotriene B4 from polymorphonuclear neutrophils induced by activators such as the calcium ionophor A23187, It also promotes the release of histamine from mast cells induced by activators such as .alpha.-toxin-producing Staphylococcus aureus cells or the calcium ionophor A23187. The peptide is effective at low concentrations within the range of 1 to 100 ppm. By promoting the release of such inflammatory mediators the peptide can potentiate the cellular immune response and stimulate the host defense against infectious disease. This newly discovered immunostimulatory agent is useful as an active component of pharmaceuticals, hygiene products, clinical foods, etc., for prevention and treatment of bacterial, fungal, and viral infectious in humans and animals.
摘要翻译： PCT No.PCT / JP92 / 00275 Sec。 371日期：1993年2月19日 102（e）日期1993年2月19日PCT提交1992年3月7日PCT公布。公开号WO93 / 18061 日本公报1993年9月16日。公开了包含衍生自乳铁蛋白的肽的免疫刺激剂，其具有调节炎症介质从免疫系统细胞释放的活性。该肽促进白三烯B4从诸如钙离子电极A23187的激活剂诱导的多形核嗜中性粒细胞的释放。它还促进由活化剂如产生α-毒素的金黄色葡萄球菌细胞或钙离子体A23187诱导的肥大细胞释放组胺。该肽在1至100ppm范围内的低浓度下是有效的。通过促进这种炎症介质的释放，肽可以增强细胞免疫应答并刺激宿主防止感染性疾病。这种新发现的免疫刺激剂可用作药物，卫生用品，临床食品等的活性成分，用于预防和治疗感染人类和动物的细菌，真菌和病毒。

33. 发明授权

US5461035A Short peptides with insulin activity 失效
标题翻译：具有胰岛素活性的短肽
公开(公告)号：US5461035A
公开(公告)日：1995-10-24
申请号：US285443
申请日：1994-08-04
申请人： Stefan Mullner , Wolfgang Konig , Gunter Muller
发明人： Stefan Mullner , Wolfgang Konig , Gunter Muller
IPC分类号： A61K38/00 , A61K38/06 , A61K38/08 , A61K38/28 , A61P3/08 , A61P3/10 , A61P43/00 , C07K1/113 , C07K5/08 , C07K5/087 , C07K5/10 , C07K7/00 , C07K7/06 , C07K14/62 , C07K5/00 , C07K17/00
CPC分类号： C07K14/62 , A61K38/00
摘要： A method for the treatment of diabetes mellitus or non-insulin-dependent diabetes comprising at least one peptide selected from the group consisting of Tyr-Gln-Leu-Glu-Asn-Tar-Cys-Asn, Acetyl-Leu-Glu-Asn-Tar-Cys-Asn OH, Asn-Tar-Cys-Asn, or a peptide of the formulaX-Q-Cys-D (II)or the stereoisomeric forms of the peptide of formula II, or the physiologically tolerated salts of the peptide of the formula II.
摘要翻译：一种治疗糖尿病或非胰岛素依赖性糖尿病的方法，包括至少一种选自Tyr-Gln-Leu-Glu-Asn-Tar-Cys-Asn，乙酰基-Leu-Glu-Asn- 焦油-Cys-Asn OH，Asn-Tar-Cys-Asn或式XQ-Cys-D（II）的肽或式II的肽的立体异构体形式，或其肽的生理学耐受盐公式二

34. 发明授权

US5326875A Alkylation of azaglycine derivatives 失效
标题翻译：阿魏酸衍生物的烷基化
公开(公告)号：US5326875A
公开(公告)日：1994-07-05
申请号：US822929
申请日：1992-01-21
申请人： Patrice Talaga , Wolfgang Konig
发明人： Patrice Talaga , Wolfgang Konig
IPC分类号： C07C281/06 , C07D213/42 , C07K1/00 , C07K5/065
CPC分类号： C07D213/42 , C07C281/06 , C07K5/06078 , Y02P20/55
摘要： A process for the preparation of alkylated azaglycine derivatives of the formula IX--(A).sub.n --N(R)--NH--CO--NH.sub.2, (I)is described in which X is an amino protective group, C.sub.1 -C.sub.8 -alkanoyl, C.sub.6 -C.sub.14 -arylcarbonyl or C.sub.6 -C.sub.14 -aryl-C.sub.1 -C.sub.4 -alkanoyl, A is amino acid or imino acid radicals optionally protected on the third function, n is 0-10, X being C.sub.1 -C.sub.8 -alkanoyl, C.sub.6 -C.sub.14 -arylcarbonyl or C.sub.6 -C.sub.14 -aryl-C.sub.1 -C.sub.4 -alkanoyl if n=0, and R is C.sub.1 -C.sub.8 -alkyl, C.sub.6 -C.sub.14 -aryl-C.sub.1 -C.sub.4 -alkanoyl or C.sub.5 -C.sub.12 -heteroaryl-C.sub.1 -C.sub.4 -alkanoyl, which comprises reacting a compound of the formula X--(A).sub.n --NH--NH--CO--NH.sub.2, in which X, A and n have the abovementioned meanings, with a primary or secondary alcohol and excess DEAD, and a tri-C.sub.1 -C.sub.6 -alkylphosphine, tri-C.sub.6 -C.sub.14 -arylphosphine or pyridyl-di-C.sub.6 -C.sub.14 -arylphosphine, it being possible for the aryl moiety to be optionally substituted by di-C.sub.1 -C.sub.4 -alkylamino, in an ether at 0.degree. C. to 30.degree. C. and optionally removing the amino protective group X, with the proviso that X is not Fmoc when tri-n-butylphosphine is used.
摘要翻译：描述了制备式I X-（A）nN（R）-NH-CO-NH 2，（I）的烷基化阿魏酸衍生物的方法，其中X是氨基保护基，C 1 -C 8 - 烷酰基，C 6 -C 14 - 芳基羰基或C 6 -C 14 - 芳基-C 1 -C 4 - 烷酰基，A是任选地在第三个功能上保护的氨基酸或亚氨基，n是0-10，X是C 1 -C 8 - 烷酰基，C 6 -C 14 - 如果n = 0，芳基羰基或C 6 -C 14 - 芳基-C 1 -C 4 - 烷酰基，并且R是C 1 -C 8 - 烷基，C 6 -C 14 - 芳基-C 1 -C 4 - 烷酰基或C 5 -C 12 - 杂芳基-C 1 -C 4 - 烷酰基其包括使X，A和n具有上述含义的式X-（A）n-NH-NH-CO-NH 2的化合物与伯醇或仲醇和过量的DEAD反应， C 1 -C 6 - 烷基膦，三-C 6 - C 14 - 芳基膦或吡啶基 - 二-C 6 - C 14 - 芳基膦，芳基部分可以任选被二C1-C4烷基氨基取代，在醚中0℃ 至30℃，任选地除去氨基保护基团X，条件是当三正丁基磷时X不是Fmoc 使用了吗啡。

35. 发明授权

US5091367A Analogs of gonadoliberin with improved solubility, methods for their preparation, agents containing them and their use 失效
标题翻译：具有改善溶解性的甘油二醇的模拟物，其制备方法，包含它们的试剂及其用途
公开(公告)号：US5091367A
公开(公告)日：1992-02-25
申请号：US724477
申请日：1991-06-28
申请人： Wolfgang Konig , Jurgen K. Sandow , Cenek Kolar
发明人： Wolfgang Konig , Jurgen K. Sandow , Cenek Kolar
IPC分类号： A61K38/00 , A61K38/04 , A61P5/00 , A61P9/12 , C07K7/06 , C07K7/23 , C07K9/00 , C07K14/575
CPC分类号： C07K7/23 , A61K38/00 , Y10S514/80
摘要： The invention relates to peptides of the formula ##STR1## in which X is absent or is hydrogen or acyl; A is Pgl, de-hydro-Pro, Pro, D-Thi or D-Pgl or represents optionally substituted D-Nal(2), D-Phe or D-Trp; B is His or optionally substituted D-Phe; C is Trp, D-Thi, D-Pal(3) or optionally substituted D-Trp; D is Tyr, Arg of His; E is D-Ser(R.sup.1), .beta.-Asn, .beta.-Asp-OMe, D-Thi or --NH--CH(CH.sub.2 R.sup.2)--CO--; F is Ser(R.sup.1), Leu, Trp or Phe; G is Gly-NH.sub.2, Aza-Gly-NH.sub.2, D-Ala-NH.sub.2 or NH-alkyl; R.sup.1 is glycosyl and R.sup.2 is hydrogen, acyl, aryl or heteroaryl.The invention also relates to methods for the preparation of these peptides, agents containing them and their use.
摘要翻译：本发明涉及式“IMAGE”的肽，其中X不存在或为氢或酰基; A是Pgl，de-hydro-Pro，Pro，D-Thi或D-Pgl或代表任选取代的D-Nal（2），D-Phe或D-Trp; B是His或任选被取代的D-Phe; C是Trp，D-Thi，D-Pal（3）或任选取代的D-Trp; D是他的Tyr，Arg; E是D-Ser（R1），β-Asn，β-Asp-OMe，D-Thi或-NH-CH（CH2R2）-CO-; F是Ser（R1），Leu，Trp或Phe; G是Gly-NH 2，Aza-Gly-NH 2，D-Ala-NH 2或NH-烷基; R1是糖基，R2是氢，酰基，芳基或杂芳基。本发明还涉及制备这些肽，含有它们的试剂及其用途的方法。

36. 发明授权

US4788178A Use of gonadoliberin and gonadoliberin agonists for the treatment of climacteric complaints 失效
标题翻译：使用生殖腺素和促性腺激素激动剂治疗更年期的投诉
公开(公告)号：US4788178A
公开(公告)日：1988-11-29
申请号：US724331
申请日：1985-04-17
申请人： Wolfgang Konig
发明人： Wolfgang Konig
IPC分类号： A61K38/04 , A61K38/09 , A61K38/22 , A61P5/00 , A61K37/02
CPC分类号： A61K38/09 , Y10S930/13
摘要： The invention relates to the use of gonadoliberin and gonadoliberin agonists for the treatment of climacteric complaints and pathological conditions in which the level of parathyroid hormone is elevated, and to preparations containing this or these compounds(s).
摘要翻译：本发明涉及促性腺激素和促性粒细胞激动剂用于治疗更年期症状和甲状旁腺激素水平升高的病理状况以及含有这些或这些化合物的制剂的用途。

37. 发明授权

US5722083A Directing a subscriber toward a destination within an SDMA mobile radio network 失效
标题翻译：将用户定向到SDMA移动无线电网络内的目的地
公开(公告)号：US5722083A
公开(公告)日：1998-02-24
申请号：US671539
申请日：1996-06-27
申请人： Wolfgang Konig
发明人： Wolfgang Konig
IPC分类号： G08G1/13 , G01C21/20 , G01S5/00 , G01S5/12 , G08G1/0968 , H04W64/00 , H04B1/00 , G01C21/00
CPC分类号： G08G1/096861 , G01C21/20 , G08G1/096872 , G08G1/096883 , H04W64/00 , G01S5/0009 , G01S5/12
摘要： A process for directing a subscriber toward a destination within an SDMA mobile radio network, and a processor-controlled facility (BSC) which operates accordingly are proposed. This facility contains a communications interface unit (IF1) for receiving a message that specifies a destination (DES) desired by a subscriber, and a microprocessor which determines the current location (LOC) of the subscriber by evaluating directional and distance information (.alpha., R). The processor-controlled facility (MSC) furthermore contains communications interface unit (IF2) whereby it retrieves information (INFO) from a data base (DB), which defines a route from the location (LOC) to the destination (DES). This information is transmitted in summary form to the subscriber's mobile radio terminal (MS).
摘要翻译：提出了一种用于将订户定向到SDMA移动无线电网络内的目的地的过程，以及相应地操作的处理器控制设施（BSC）。该设施包括用于接收指定用户所期望的目的地（DES）的消息的通信接口单元（IF1）以及通过评估方向和距离信息（α，R）来确定用户的当前位置（LOC）的微处理器）。处理器控制设施（MSC）还包含通信接口单元（IF2），从而从数据库（DB）检索信息（INFO），数据库（DB）定义从位置（LOC）到目的地（DES）的路由。该信息以概要形式传送到用户的移动无线电终端（MS）。

38. 发明授权

US5434138A Gonadoliberin antagonists 失效
标题翻译： Gonadoliberin拮抗剂
公开(公告)号：US5434138A
公开(公告)日：1995-07-18
申请号：US151056
申请日：1993-11-12
申请人： Wolfgang Konig , Jurgen Sandow , Cenek Kolar
发明人： Wolfgang Konig , Jurgen Sandow , Cenek Kolar
IPC分类号： A61K38/00 , A61P5/00 , A61P5/24 , C07K7/06 , C07K7/23 , C07K9/00 , C07K14/575 , C07K7/00
CPC分类号： C07K7/23 , A61K38/00
摘要： Peptides of the formula ##STR1## in which X is alkanoyl, A is optionally substituted D-Nal(2), D-Phe or D-Trp, B is optionally substituted D-Phe, C is D-Pal(3) or optionally substituted D-Phe or D-Trp, and D is Tyr or His, E is D-Ser (R.sup.1), F is Leu, Trp or Phe, G is L-Ser(R.sup.1), H is Gly-NH.sub.2, D-Ala-NH.sub.2 or Azagly-NH.sub.2 and R.sup.1 is a glycosyl radical. These peptides have an inhibitory effect on the formation of the gonadotropins lutropin and follitropin and thus also on the synthesis of testo-sterone and estrogen. A process for the preparation of these peptides is described.
摘要翻译：式中，X为链烷酰基，A为任选取代的D-Nal（2），D-Phe或D-Trp，B为任选取代的D-Phe，C为D-Pal（3）或任选地为取代的D-Phe或D-Trp，D为Tyr或His，E为D-Ser（R1），F为Leu，Trp或Phe，G为L-Ser（R1），H为Gly-NH2， Ala-NH2或Azagly-NH2，R1是糖基。这些肽对促性腺激素营养素和叶黄素的形成具有抑制作用，因此也对睾酮和雌激素的合成具有抑制作用。描述了制备这些肽的方法。

39. 发明授权

US5071836A Competitive gonadoliberin antagonists 失效
标题翻译：竞争性GONADOLIBERIN拮抗剂
公开(公告)号：US5071836A
公开(公告)日：1991-12-10
申请号：US448904
申请日：1989-12-12
申请人： Cenek Kolar , Wolfgang Konig , Jurgen K. Sandow
发明人： Cenek Kolar , Wolfgang Konig , Jurgen K. Sandow
IPC分类号： A61K38/04 , A61K38/00 , A61P5/00 , C07K7/23
CPC分类号： C07K7/23 , A61K38/00
摘要： Peptides of the formulaAc-D-Nal(2)-D-Phe-D-Phe-Ser-X-D-Ser(Rha)-Leu-Arg-Pro-Yin which X represents Tyr or His and Y represents Gly-NH.sub.2, D-Ala-NH.sub.2, Azgly-NH.sub.2 or NH--C.sub.2 H.sub.5 are competitive antagonists of Gn-RH. They are used for the treatment of gonadotropin- and steroid-dependent diseases and are prepared by known methods of peptide chemistry.
摘要翻译：式Ac-D-Nal（2）-D-Phe-D-Phe-Ser-XD-Ser（Rha）-Leu-Arg-Pro-Y的肽，其中X表示Tyr或His，Y表示Gly-NH2 ，D-Ala-NH2，Azgly-NH2或NH-C2H5是Gn-RH的竞争性拮抗剂。它们用于治疗促性腺激素和类固醇依赖性疾病，并通过已知的肽化学方法制备。

40. 发明授权

US4711847A Preparation of secretin 失效
标题翻译：泌乳素的制备
公开(公告)号：US4711847A
公开(公告)日：1987-12-08
申请号：US638789
申请日：1984-08-08
申请人： Wolfgang Konig , Joachim Engels , Eugen Uhlmann , Waldemar Wetekam
发明人： Wolfgang Konig , Joachim Engels , Eugen Uhlmann , Waldemar Wetekam
IPC分类号： C12N15/09 , A61K38/22 , C07H21/04 , C07K14/005 , C07K14/195 , C07K14/575 , C07K14/645 , C07K19/00 , C12N1/20 , C12N15/62 , C12P21/02 , C12R1/19 , C12N9/78 , C12N15/00 , C12P21/06
CPC分类号： C12N15/62 , C07K14/645 , C07K2319/00 , C07K2319/61 , C07K2319/75
摘要： Secretin, which cannot be prepared directly by genetic engineering because of its carboxylic acid carboxyl-terminus, can be obtained by preparing secretylglycine by genetic engineering and then obtaining secretin therefrom by enzymatic conversion of the terminal glycine radical. The gene for the secretylglycine is synthesized chemically from smaller single-stranded units which are linked enzymatically to give the complete gene, incorporated into a suitable vector and amplified therein, after which the peptide is isolated directly or as a fusion protein and, after cyanogen bromide cleavage, is converted enzymatically into secretin.
摘要翻译：由于其羧酸羧基末端，不能通过基因工程直接制备的神经肽可以通过基因工程制备分泌甘氨酸，然后通过末端甘氨酸基因的酶转化获得分泌素。分泌甘氨酸的基因由较小的单链单元进行化学合成，该单链单元被酶促连接以产生完整的基因，并入合适的载体并在其中扩增，之后直接或作为融合蛋白分离肽，并且在溴化氰切割，酶促转化成促胰液素。

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